CA2840029C - Derives d'oxazole et de thiazole comme inhibiteurs selectifs de proteines kinases (c-kit) - Google Patents

Derives d'oxazole et de thiazole comme inhibiteurs selectifs de proteines kinases (c-kit) Download PDF

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Publication number
CA2840029C
CA2840029C CA2840029A CA2840029A CA2840029C CA 2840029 C CA2840029 C CA 2840029C CA 2840029 A CA2840029 A CA 2840029A CA 2840029 A CA2840029 A CA 2840029A CA 2840029 C CA2840029 C CA 2840029C
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methyl
oxazol
disease
optionally substituted
phenylamino
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CA2840029A1 (fr
Inventor
Abdellah Benjahad
Alain Moussy
Emmanuel Chevenier
Willy Picoul
Anne Lermet
Didier Pez
Jason Martin
Franck Sandrinelli
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AB Science SA
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AB Science SA
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/00—Medicinal preparations containing organic active ingredients
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/00—Medicinal preparations containing organic active ingredients
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems

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  • Health & Medical Sciences (AREA)
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  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
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  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
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  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychology (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

L'invention concerne des composés représentés par la formule I, ou des sels pharmaceutiquement acceptables de ceux-ci. Dans la formule, R1, R2, R3, A, Q, W et X sont tels que définis dans le descriptif. Ces composés modulent, régulent et/ou inhibent sélectivement la transduction de signal facilitée par certaines protéines kinases natives et/ou mutantes impliquées dans diverses maladies humaines et animales, telles que des troubles de la prolifération cellulaire, des troubles métaboliques, allergiques et dégénératifs. Plus particulièrement, ces composés constituent de puissants inhibiteurs sélectifs de c-kit native et/ou mutante.
CA2840029A 2011-07-27 2012-07-24 Derives d'oxazole et de thiazole comme inhibiteurs selectifs de proteines kinases (c-kit) Expired - Fee Related CA2840029C (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161512165P 2011-07-27 2011-07-27
US61/512,165 2011-07-27
PCT/EP2012/064539 WO2013014170A1 (fr) 2011-07-27 2012-07-24 Dérivés d'oxazole et de thiazole comme inhibiteurs sélectifs de protéines kinases (c-kit)

Publications (2)

Publication Number Publication Date
CA2840029A1 CA2840029A1 (fr) 2013-01-31
CA2840029C true CA2840029C (fr) 2021-07-20

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ID=46601793

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CA2840029A Expired - Fee Related CA2840029C (fr) 2011-07-27 2012-07-24 Derives d'oxazole et de thiazole comme inhibiteurs selectifs de proteines kinases (c-kit)

Country Status (17)

Country Link
US (1) US9168245B2 (fr)
EP (1) EP2736904B1 (fr)
JP (1) JP5944503B2 (fr)
KR (1) KR101924247B1 (fr)
CN (1) CN103717591B (fr)
AR (1) AR087354A1 (fr)
AU (1) AU2012288900B2 (fr)
BR (1) BR112014001977A2 (fr)
CA (1) CA2840029C (fr)
CL (1) CL2014000007A1 (fr)
ES (1) ES2573831T3 (fr)
IL (1) IL230504A0 (fr)
MX (1) MX2014001079A (fr)
RU (1) RU2612972C2 (fr)
TW (1) TW201311676A (fr)
WO (1) WO2013014170A1 (fr)
ZA (1) ZA201400465B (fr)

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AU2012288900A1 (en) 2014-01-16
ZA201400465B (en) 2015-04-29
TW201311676A (zh) 2013-03-16
KR20140041609A (ko) 2014-04-04
KR101924247B1 (ko) 2019-02-22
BR112014001977A2 (pt) 2017-02-21
EP2736904A1 (fr) 2014-06-04
CN103717591A (zh) 2014-04-09
US9168245B2 (en) 2015-10-27
AR087354A1 (es) 2014-03-19
CL2014000007A1 (es) 2014-09-05
ES2573831T3 (es) 2016-06-10
US20140179698A1 (en) 2014-06-26
RU2612972C2 (ru) 2017-03-14
EP2736904B1 (fr) 2016-03-16
JP5944503B2 (ja) 2016-07-05
IL230504A0 (en) 2014-03-31
WO2013014170A1 (fr) 2013-01-31
RU2014107463A (ru) 2015-09-10
AU2012288900B2 (en) 2016-10-06
JP2014521624A (ja) 2014-08-28
CA2840029A1 (fr) 2013-01-31
MX2014001079A (es) 2014-09-12

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